Novartis Ag

Emisphere Technologies, Inc.

Novartis Pharma Gmbh

Joseph Sikora

Simon David Bateman

Joseph Ault

Moise Azria

Michael M Goldberg

Rajesh K Agarwal

Kiran Chaudhary

Subash Patel

Rebecca F Yang

Joseph Zielinski

Shingai Majuru

JoAnne P Corvino

William Elliot Bay

William Elliott Bay

Gregory Sparta

Rebecca Fai-ying Yang

Jie Xiao

Shingai Majura

JoAnne P Russo

Mosise Azria

Joanne P Russo

Joseph Murray Ault

Joseph L Zielinski

Rebecca Fai-Ying Yang

Joseph M Ault

The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. Preferred delivery agents include, but are not limited to, N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC), N-(10-[2-hydroxybenzoyl]amino)decanoic acid (SNAD), and sodium N-(8-[2-hydroxybenzoyl]amino)caprylate (SNAC). The invention also provides methods of preparing the disodium salt, ethanol solvate, and hydrate and compositions containing the disodium salt, ethanol solvate, and/or hydrate.

Disodium salts, monohydrates, and ethanol solvates for delivering active agents

The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have the formula wherein

Solid pharmaceutical compositions suitable for the oral delivery of pharmacologically active agents, e.g. peptides, comprising a therapeutically-effective amount of a pharmacologically active agent; a crospovidone or povidone; and a delivery agent for said pharmacologically active agent are disclosed. The compositions provide excellent oral bioavailability of pharmacologically active agents, particularly calcitonin.

Pharmaceutical compositions for the oral delivery of pharmacologically active agents

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Succasunna, NJ, United States of America

Joseph Sikora